Synthesis and cytotoxic activity of novel 3-methyl-1-[(4-substitutedpiperazin-1-yl)methyl]-1 H-indole derivatives

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dc.citation.epage394en_US
dc.citation.issueNumber8en_US
dc.citation.spage389en_US
dc.citation.volumeNumber62en_US
dc.contributor.authorKoksal, M.en_US
dc.contributor.authorYarim, M.en_US
dc.contributor.authorDurmaz, I.en_US
dc.contributor.authorCetin Atalay, R.en_US
dc.date.accessioned2016-02-08T09:45:24Z
dc.date.available2016-02-08T09:45:24Z
dc.date.issued2012en_US
dc.departmentDepartment of Molecular Biology and Geneticsen_US
dc.description.abstractA series of novel 3-methyl-1-[(4-substitutedpiperazin-1-yl)methyl]-1H- indoles (3a-l) were synthesized and their cytotoxicities were analyzed against 3 different human cell lines, including liver (HUH7), breast (MCF7) and colon (HCT116). The Mannich reaction of 3-methylindole (1) with 4- substitutedpiperazines (2) and formaldehyde resulted to the 3-methyl-1-[(4- substitutedpiperazin-1-yl)methyl]-1H-indoles (3a-l) in 38-69% yields. The investigation of anticancer screening revealed that the tested compounds showed comparable activity to the reference drug 5-fluorouracil and compounds 3g, 3h, 3i and 3k, had lower 50% inhibition (IC 50) concentration than reference drug. Moreover, the cytotoxic effect of the most potent compound 3h on HUH7 and MCF7 cells through apoptosis was visualized by Hoechst staining and compared with paclitaxel, which is a mitotic inhibitor acting on microtubules. The morphological features of apoptosis were observed as condensed and fragmented nuclei that are similar to paclitaxel. © Georg Thieme Verlag KG Stuttgart.New York.en_US
dc.description.provenanceMade available in DSpace on 2016-02-08T09:45:24Z (GMT). No. of bitstreams: 1 bilkent-research-paper.pdf: 70227 bytes, checksum: 26e812c6f5156f83f0e77b261a471b5a (MD5) Previous issue date: 2012en
dc.identifier.doi10.1055/s-0032-1314868en_US
dc.identifier.issn0004-4172
dc.identifier.urihttp://hdl.handle.net/11693/21372
dc.language.isoEnglishen_US
dc.publisherThiemeen_US
dc.relation.isversionofhttp://dx.doi.org/10.1055/s-0032-1314868en_US
dc.source.titleArzneimittel-Forschung/Drug Researchen_US
dc.subjectAnticanceren_US
dc.subjectApoptosisen_US
dc.subjectIndoleen_US
dc.subjectMannich baseen_US
dc.titleSynthesis and cytotoxic activity of novel 3-methyl-1-[(4-substitutedpiperazin-1-yl)methyl]-1 H-indole derivativesen_US
dc.typeArticleen_US

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